Write an essay about Sitagliptin.

Answer to Question: 300884 Pharmacology

Sitagliptin is an antihyperglycemic/antidiabetic drug used to manage Type 2 Diabetic Mellitus (Inamdar, Mhaske 2012).

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Merck & Co. discovered this drug and it is used for patients with Type 2 Diabetes Mellitus (Inamdar and Mhaske 2012). 2013).

This drug was first developed in 2006. It was approved by US Food and Drug administration October 17th 2006.

Merck and Co., a company based in Merck and Co., approved marketing the drug on April 2, 2007. 2012).

Sitagliptin and other drugs were combined to provide positive results in patients suffering from T2D.

Janumet also sold this drug, which contained Sitagliptin as well as metformin.

The physical properties and molecular formulas of the active pharmaceutical component and its chemical form

Januvia’s molecular formula is C16H15F6N5O. (Inamdar, Mhaske 2012).

Sitagliptin Phosphate monhydrate is the active pharmaceutical ingredients of this drug. This is a powdery, off-white, hygroscopic material that dissolves in water. The chemical formula of the active pharmaceutical ingredient is C16H15F6N5O*H3PO4*H2O.

The physical properties of drug should be discussed, including its chiral center, solubility as well as molecular weight and melting points.

Russell-Jones, et. al., reported that the drug’s melting temperature is between 216 and 219.32°C, and its molecularweight is 407.32 grams/mol. Meanwhile, the solubility is 179.2 grams/L of water at 25°C (Russell Jones). 2012).

The drug comes in a liquid form and is viscous in color.

It is important that you mention the stability of your drug. It can be stored in accordance to directions and without strong oxidizing agent.

Also, thermal decomposition should be avoided as it can cause toxic gases like carbon monoxide and other poisonous gases (Sin Mahe & Sigal 2012).

Crystallization properties of the API

In addition, Sin, Mahe, Sigal (2012) should discuss the characteristics of crystallization for the API of this drug.

The crystallization process is made up of crystal salts that form monophosphate versions of the drug.

Four variants of drug crystallized varieties are currently available, all patentable and ready to be used for patients.

These salts of a drug with their solvates and hydrates and polymorphic forms provide high bioavailability and reduce decomposition and hydrolysis (Ghislieri and al. 2013).

Administration Routes and Dosage forms with Pharmacokinetic Data

Patients with type 1 and type 2 diabetes should not have this drug. They should receive it as tablets in strengths 25 mg, 50 mg, and 100 mg (Sin Mahe, Sigal, 2012).

Inamdar (2012) and Mhaske (2012) state that oral doses are the most effective for maintaining the body’s enzyme balance.

Sitagliptin has a pharmacokinetic profile that allows for easy absorption. The half-life inside the body is between 8 and 14 hours.

Russell-Jones et. al. found that more then 80% of the drug is excreted in excretion. This means that the drug works according to the dose. 2012).

Description of The Formulation

The drug is available in tablet form with many benefits and some drawbacks.

One advantage is its oral administration, which reduces hyperglycemia.

Additionally, sitagliptin is not associated with weight gain, so it is safe and appropriate treatment for patients suffering from type 2 diabetes (Ghislieri-et al. 2013).

Description of manufacturing stepsThe synthesis process of Sitagliptin is an organic synthesis process which includes the formation of a liquid compound 5-hydroxyl-[(2,4,5-trifluoro-phenyl)-ethylidene]-dimethyl-[1,3] dioxo-4,6-diketone from the 2,4,5-trifluoro-phenylacetic acid, meldrum’s acid, N,N-diisopropylethylamine, DMAP and acetylchloride; adding 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4] triazol [4,3-alpha] pyrazine hydrochloride and trifluoroacetic acid (Inamdar and Mhaske 2012).

This is the step that results in the final pharmacological product.

Refer to

Ghislieri D. Green A.P. Pontini M. Willies S.C. Rowles I. Frank A. Grogan G. Turner N.J. 2013.

Engineering an antiselective amine oxygenase for the production of pharmaceutical building blocks, alkaloid natural product and other chemical compounds.

Journal of the American Chemical Society. 135 (29), pp.10863 -10869.Inamdar, H.P.

Mhaske A.A. and Inamdar, H.P. RP-HPLC method for simultaneous determination of Metformin Hydrochloride, Rosiglitazone and Sitagliptin-application to commercially available Drug Products.

International Journal of Pharmaceutical Sciences and Research.Russell-Jones, D., Cuddihy, R.M., Hanefeld, M., Kumar, A., Gonzalez, J.G., Chan, M., Wolka, A.M., Boardman, M.K.

2012 DURATION-4 Study Group.

Exenatide’s safety and efficacy in monotherapy of type 2 diabetes in drug-naive patients (DURATION-4): a 26-week, double-blind trial.

Diabetes care 35(2), pp. 252-258.

Sin, C.Mahe, E., Sigal, M.L. 2012

Patient receiving sitagliptin had an adverse drug reaction (DRESS), which included eosinophilia, systemic symptoms, and Mahe, E.

Diabetes & metabolism, 38(6) pp.571-573.

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